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US 2020/0392111 A1Published application
Method for preparing tyrosine kinase inhibitor and derivative thereof
AssigneeJiangsu Hengrui Medicine Co., Ltd.
InventorsGuaili Wu, Quanliang Zhang, Yongxing Cao
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Abstract
A method for preparing a tyrosine kinase inhibitor and a derivative thereof are described. In particular, the present method has a short synthesis route, low costs, easy operation, and is suitable for large-scale production.
Claims4
A compound of formula VI,
- wherein R2 is selected from the group consisting of hydrogen, an amino protecting group, cycloalkyl, cycloalkenyl, alkyl, alkenyl, alkynyl, aralkyl, and substituted or unsubstituted aryl or heteroaryl;
- R is selected from the group consisting of hydroxy, —ORa, and halogen;
- and
- Ra is selected from the group consisting of alkyl, aryl, and alkylaryl, wherein the alkyl, aryl, and alkylaryl are each optionally substituted by a substituent.
1 more element
A method for preparing a compound of formula VI, comprising a Wittig-Horner reaction between a compound of formula VIII and phosphoryl carboxylate to obtain a compound of formula X,
- wherein R2 is selected from the group consisting of hydrogen, an amino protecting group, cycloalkyl, cycloalkenyl, alkyl, alkenyl, alkynyl, aralkyl, and substituted or unsubstituted aryl or heteroaryl;
- R is selected from the group consisting of hydroxy, —ORa, and halogen;
- and
- Ra is selected from the group consisting of alkyl, aryl, and alkylaryl, wherein the alkyl, aryl, and alkylaryl are each optionally substituted by a substituent, and the phosphoryl carboxylate is triethyl phosphonoacetate.
1 more element
Dependencies are inferred from the claim text.